Author, as appears in the article.: López-Suárez L; Riesgo L; Bravo F; Ransom T; Beutler J; Echavarren A
Department: Química Analítica i Química Orgànica
URV's Author/s: ECHAVARREN PABLOS, ANTONIO
Keywords: Tumor growth inhibition Renal cancer Natural products Gold catalysis Englerin a Enantioselective synthesis
Abstract: © 2016 The Authors. We report the synthesis and biological evaluation of a series of (-)-englerin A analogues obtained along our previously reported synthetic route based on a stereoselective gold(I) cycloaddition process. This synthetic route is a convenient platform to access analogues with broad structural diversity and has led us to the discovery of unprecedented and easier-to-synthesize derivatives with an unsaturation in the cyclopentyl ring between C4 and C5. We also introduce novel analogues in which the original isopropyl motif has been substituted with cyclohexyl, phenyl, and cyclopropyl moieties. The high selectivity and growth-inhibitory activity shown by these new derivatives in renal cancer cell lines opens new ways toward the final goal of finding effective drugs for the treatment of renal cell carcinoma (RCC).
Thematic Areas: Saúde coletiva Química Pharmacology, toxicology and pharmaceutics (miscellaneous) Pharmacology, toxicology and pharmaceutics (all) Pharmacology & pharmacy Pharmacology Organic chemistry Odontología Molecular medicine Medicina ii Medicina i Materiais Interdisciplinar General pharmacology, toxicology and pharmaceutics General medicine Farmacia Drug discovery Ciências biológicas iii Ciências biológicas ii Ciências biológicas i Ciências ambientais Chemistry, medicinal Biotecnología Biochemistry
licence for use: https://creativecommons.org/licenses/by/3.0/es/
Author's mail: antoniomaria.echavarren@urv.cat
Author identifier: 0000-0002-6418-7930
Record's date: 2024-10-26
Papper version: info:eu-repo/semantics/publishedVersion
Papper original source: Chemmedchem. 11 (9): 1003-1007
APA: López-Suárez L; Riesgo L; Bravo F; Ransom T; Beutler J; Echavarren A (2016). Synthesis and Biological Evaluation of New (-)-Englerin Analogues. Chemmedchem, 11(9), 1003-1007. DOI: 10.1002/cmdc.201600040
Licence document URL: https://repositori.urv.cat/ca/proteccio-de-dades/
Entity: Universitat Rovira i Virgili
Journal publication year: 2016
Publication Type: Journal Publications
Repositori URV